XSJ151 

XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer^[1].

XSJ151 (48 h) exhibits strong cytotoxicity against gastric cancer cell lines, including AGS (IC₅₀ = 0.088 μM), MGC803 (IC₅₀ = 0.592 μM), HGC27 (IC₅₀ = 1.951 μM), and SGC7901 (IC₅₀ = 11.121 μM), while showing lower cytotoxicity against normal cell lines such as GES-1 (IC₅₀ = 0.202 μM) and HIEC (IC₅₀ > 40 μM)^[1].
XSJ151 (0.1-2.5 nM, 7-10 days) inhibits gastric cancer cell colony formation in a concentration-dependent manner. In AGS cells, 2.5 nM XSJ151 reduces the colony count from 74 to 22; in MGC803 cells, it reduces it from 68 to 21^[1].
XSJ151 (2.5-10 nM, 24 h) dose-dependently induces G2/M phase arrest in AGS and MGC803 gastric cancer cells, leading to significant enrichment of the G2/M-phase population^[1].
XSJ151 (44-600 nM, 48 h) significantly upregulates the expression of G2/M phase-related proteins (p53, p21, CCNB) and the S phase marker CCNA in AGS and MGC803 cells, while the G1 phase-specific protein CCNE is downregulated in a dose-dependent manner^[1].
XSJ151 (88–600 nM, 48 h) induces apoptosis in AGS and MGC803 cells by significantly upregulating BAD and BAX proteins and downregulating Bcl-2 protein^[1].
XSJ151 (88-600 nM, 48 h) significantly increases the number of γ-H2AX intranuclear spots in AGS and MGC803 cells, indicating DNA double-strand breaks and significantly increased γ-H2AX protein levels^[1].
XSJ151 (150-200 μM, 30 min) effectively inhibits Topo I-catalyzed DNA relaxation^[1].
XSJ151 (44-600 μM, 48 h) significantly downregulates Topo I protein in AGS and MGC803 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

737.73

C₃₇H₃₁N₅O₁₀S

1685279-23-5

COC(C=C1)=CC=C1CC(NCC(O[C@]2(CC)C(OCC3=C2C=C4N(CC5=CC6=CC=CC=C6N=C54)C3=O)=O)=O)=NS(C7=CC=C([N+]([O-])=O)C=C7)(=O)=O

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• [1]. Si Z, et al. Camptothecin 20(S)-sulfonyl amidine derivative inhibits gastric cancer cell proliferation by targeting topoisomerase I to trigger the DNA damage-apoptosis cascade. Bioorg Chem. 2025 Nov;166:109171.  [Content Brief]